栀子苷在血管性痴呆及正常大鼠大脑皮层的药动学研究

Pharmacokinetics of geniposide in the cerebral cortex of vascular dementia and normal rats

目的:研究栀子苷在正常和血管性痴呆大鼠大脑皮层的药动过程。方法:尾静脉注射300 mg·kg-1栀子苷,给药后2,5,10,15,30,45,60,90,120 min断头取大脑皮层,用RP-HPLC法测定栀子苷在大脑皮层的含量,应用DAS 2.11统计软件模拟计算,得出相应的药动学参数。结果:栀子苷在正常及血管性痴呆大鼠大脑皮层药动学符合二室开放模式,正常组和血管性痴呆组的AUC0-t分别为(46.41±6.34)和(58.56±7.17)μg·min·mL-1;MRT分别为(38.16±5.87)和(38.34±4.96)min;C max分别为(1.29±0.42)和(1.61±0.26)μg·mL-1。结论:栀子苷在大脑皮层以消除为主;与正常组比较,栀子苷在血管性痴呆大鼠体内停留时间更长,消除更慢。

Objective： To investigate the pharmacokinetics of geniposide in the cerebral cortex of vascular dementia and normal rats. Methods： At 2, 5, 10, 15, 30, 45, 60, 90 and 120 min after intravenous injection of geniposide （300 mg·kg^-1 ） , the cerebral cortex was collected from rats. The concentration of geniposide in the cer- ebral cortex was detected by RP-HPLC, and the pharmacokinetic parameters of geniposide were analyzed by DAS 2.11 software. Results： Pharmacokinetic of geniposide in the cerebral cortex was accorded with two-compartment model. The pharmacokinetics of geuiposide in the cerebral cortex was accorded with two-compartment model. AUC0-t, was （46.41 ±6.34） and （58.56±7.17） μg·min·mL^-1 in normal and vascular dementia groups, respec- tively. MRT was （38.16±5.87） and （38.34 ±4.96） rain; and Cmax was （1.29 ±0.42） and （1.61 ±0.26）μg· mL^-1 , respectively. Conclusion： Geniposide is eliminated mainly in the brain cortex. It stays longer and is e- liminated more slowly in vascular dementia rats that in normal rats.